Comparison of the CLin,u determined by LESA and the CLin,u calculated at two different microsomal protein concentrations using fu values determined by equilibrium dialysis, ultrafiltration, and ultracentrifugation
Clearances are expressed as μl/min/mg microsomal protein. Values represent the mean ± S.E. of triplicate determinations.
Drug | CLin,u | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| LESA | Equilibrium Dialysis | Ultracentrifugation | Ultrafiltration | ||||||||||
| 1 mg/ml | 0.2 mg/ml | 1 mg/ml | 0.2 mg/ml | 1 mg/ml | 0.2 mg/ml | ||||||||
| Desipramine | 41 ± 12 | 47 ± 4 | 32 ± 5 | 34 ± 1 | 34 ± 3 | 32 ± 2 | 35 ± 3 | ||||||
| Amitryptiline | 108 ± 4 | 63 ± 18 | 86 ± 6 | 131 ± 8 | 99 ± 5 | 107 ± 7 | 119 ± 6 | ||||||
| Imipramine | 59 ± 6 | 54 ± 12 | 53 ± 11 | 35 ± 2 | 39 ± 3 | 52 ± 3 | 58 ± 4 | ||||||
| Verapamil | 222 ± 15 | 223 ± 18 | 256 ± 38 | 175 ± 16 | 170 ± 10 | 197 ± 10 | 210 ± 12 | ||||||
| Diltiazem | 38 ± 4 | 28 ± 6 | 34 ± 2 | 34 ± 2 | 29 ± 1 | 32 ± 2 | 30 ± 1 | ||||||
| Propafenone | 185 ± 21 | 114 ± 7 | 171 ± 18 | 116 ± 7 | 150 ± 10 | 127 ± 8 | 171 ± 11 | ||||||
| Chlorpromazine | 191 ± 33 | 338 ± 27 | 353 ± 52 | 195 ± 9 | 167 ± 3 | N.D. | N.D. | ||||||
| Midazolam | 333 ± 11 | 364 ± 26 | 325 ± 35 | 316 ± 19 | 285 ± 20 | 347 ± 24 | 325 ± 23 | ||||||
| Diclofenac | 344 ± 24 | 252 ± 9 | 366 ± 28 | 363 ± 21 | 395 ± 34 | 372 ± 22 | 415 ± 35 | ||||||
N.D., not determined.